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Synthesis of [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818; two potential radioligands for the dopamine transporter

Journal Article:

Abstract

The preparation of no-carrier-added {sup 18}F labelled NNC 12-0817 (1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-[4-oxo-4-(2-thienyl)bu tyl]piperazine) and NNC 12-0818 (1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-[4-hydroxy-4-(2-thienyl )butyl] piperazine) is described. NNC 12-0818 is the designation of the racemic mixture of two enantiomers. Fluorine-18 is introduced into 4-[{sup 18}F]fluoro-4`-fluorobenzophenone from the corresponding triflate salt by a nucleophilic aromatic substitution reaction. A no-carrier-added synthesis was performed in 6 steps starting from N,N-dimethylaniline and 4-fluorobenzoyl chloride giving [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818 in good yields and a radiochemical purity after HPLC-purification higher than 99%. (author).
Authors:
Mueller, Lars; Foged, Christian; Hohlweg, Rolf; [1]  Halldin, Christer [2] 
  1. Novo Nordisk A/S, Maaloev (Denmark). Pharmaceuticals Div.
  2. Karolinska Inst., Stockholm (Sweden). Dept. of Clinical Neuroscience
Publication Date:
May 01, 1995
Product Type:
Journal Article
Reference Number:
SCA: 400703; PA: AIX-26:062459; EDB-95:125033; SN: 95001457630
Resource Relation:
Journal Name: Applied Radiation and Isotopes; Journal Volume: 46; Journal Issue: 5; Other Information: PBD: May 1995
Subject:
40 CHEMISTRY; ORGANIC FLUORINE COMPOUNDS; FLUORINE 18; LABELLING; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; CHEMICAL REACTION YIELD; DOPAMINE; IN VIVO; PIPERAZINES
OSTI ID:
97804
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: ARISEF; ISSN 0883-2889; TRN: GB9501280062459
Submitting Site:
GBN
Size:
pp. 323-328
Announcement Date:

Journal Article:

Citation Formats

Mueller, Lars, Foged, Christian, Hohlweg, Rolf, and Halldin, Christer. Synthesis of [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818; two potential radioligands for the dopamine transporter. United Kingdom: N. p., 1995. Web.
Mueller, Lars, Foged, Christian, Hohlweg, Rolf, & Halldin, Christer. Synthesis of [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818; two potential radioligands for the dopamine transporter. United Kingdom.
Mueller, Lars, Foged, Christian, Hohlweg, Rolf, and Halldin, Christer. 1995. "Synthesis of [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818; two potential radioligands for the dopamine transporter." United Kingdom.
@misc{etde_97804,
title = {Synthesis of [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818; two potential radioligands for the dopamine transporter}
author = {Mueller, Lars, Foged, Christian, Hohlweg, Rolf, and Halldin, Christer}
abstractNote = {The preparation of no-carrier-added {sup 18}F labelled NNC 12-0817 (1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-[4-oxo-4-(2-thienyl)bu tyl]piperazine) and NNC 12-0818 (1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-[4-hydroxy-4-(2-thienyl )butyl] piperazine) is described. NNC 12-0818 is the designation of the racemic mixture of two enantiomers. Fluorine-18 is introduced into 4-[{sup 18}F]fluoro-4`-fluorobenzophenone from the corresponding triflate salt by a nucleophilic aromatic substitution reaction. A no-carrier-added synthesis was performed in 6 steps starting from N,N-dimethylaniline and 4-fluorobenzoyl chloride giving [{sup 18}F]NNC 12-0817 and [{sup 18}F]NNC 12-0818 in good yields and a radiochemical purity after HPLC-purification higher than 99%. (author).}
journal = {Applied Radiation and Isotopes}
issue = {5}
volume = {46}
journal type = {AC}
place = {United Kingdom}
year = {1995}
month = {May}
}